Complexants for the clathration mediated synthesis of the antibiotic cephradine

Abstract

Enzymatic synthesis of cephalosporins is hampered by secondary hydrolysis and by complicated down-stream processing. Instantaneous removal of cephalosporin product by clathration, using an efficient and selective complexing agent, offers an attractive opportunity to tackle these problems. A series of benzene derivatives that form clathrate-type complexes with the cephalosporin antibiotics was subjected to efficiency measurements with Cephradine and enzyme inhibition studies. The best results for the antibiotic Cephradine were obtained with methyl 2-aminobenzoate, 2-hydroxybiphenyl and methyl 4-hydroxybenzoate. These three compounds are environmentally and toxicologically fully acceptable for application in a ‘green’ process.